231287-74-4Relevant academic research and scientific papers
Intermolecular Reductive C-N Cross Coupling of Nitroarenes and Boronic Acids by PIII/PV=O Catalysis
Nykaza, Trevor V.,Cooper, Julian C.,Li, Gen,Mahieu, Nolwenn,Ramirez, Antonio,Luzung, Michael R.,Radosevich, Alexander T.
supporting information, p. 15200 - 15205 (2018/11/30)
A main group-catalyzed method for the synthesis of aryl- and heteroarylamines by intermolecular C-N coupling is reported. The method employs a small-ring organophosphorus-based catalyst (1,2,2,3,4,4-hexamethylphosphetane) and a terminal hydrosilane reductant (phenylsilane) to drive reductive intermolecular coupling of nitro(hetero)arenes with boronic acids. Applications to the construction of both Csp2-N (from arylboronic acids) and Csp3-N bonds (from alkylboronic acids) are demonstrated; the reaction is stereospecific with respect to Csp3-N bond formation. The method constitutes a new route from readily available building blocks to valuable nitrogen-containing products with complementarity in both scope and chemoselectivity to existing catalytic C-N coupling methods.
PROTEIN KINASE INHIBITORS
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Paragraph 0192, (2015/02/18)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
PROTEIN KINASE INHIBITORS
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Page/Page column 50, (2013/04/25)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
AMINOPYRIMIDINES AS SYK INHIBITORS
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, (2011/07/07)
The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
Efficient synthesis of 1,3,5-trisubstituted benzenes via three Pd-mediated carbon-sulfur, carbon-nitrogen and carbon-carbon bond formation reactions
Liu, Bin,Shetty, Rupa S.,Moffett, Kristofer K.,Kelly, Martha J.
experimental part, p. 1680 - 1684 (2011/04/26)
An efficient synthesis of 1,3,5-trisubstituted benzenes via a sequential Pd-mediated carbon-sulfur, carbon-nitrogen, and carbon-carbon bond formation reactions is reported. Selective amidation and sulfonamidation reactions are accomplished via Pd-catalyze
5-HT6 receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides
Boes, Michael,Sleight, Andrew J.,Godel, Thierry,Martin, James R.,Riemer, Claus,Stadler, Heinz
, p. 165 - 178 (2007/10/03)
RO-04-6790 (6a) has been identified in a random screen for 5-HT6 receptor antagonists. In a medicinal chemistry optimisation program a series of analogs comprising N-heteroaryl- and N-arylbenzenesulfonamides have been synthesised and investigated for their binding affinity. Compounds with a log D profile indicative of brain penetration have been subjected to in vivo testing for reversal of a scopolamine-induced retention deficit in a passive avoidance paradigm.
BENZOSULFONE DERIVATIVES
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, (2008/06/13)
The present invention relates to novel compounds of the general formula STR1 wherein R 1 is hydrogen;R. sup.2 is hydrogen, trifluoromethyl or lower alkyl;R 3 is hydrogen or amino; or R 1 and R 2 or R 3 and R 2 taken together are--CH. dbd.CH--CH=CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R 4, R 5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C. sub.3-C 6 cycloalkyl, C 3-C 6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group--NH(CH. sub.2). sub.n NR 6 R 7,--N(CH 3)(CH 2) n NR 6 R. sup.7,--NH(CH 2) n-morpholin-4-yl or--NH(CH 2) n OH; n is 2-4R 6 and R 7 are each independently hydrogen or lower alkyl,and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.
